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Self-Liganded Suzuki–Miyaura Coupling for Site-Selective Protein PEGylation

Authors


  • We thank the Swiss National Science Foundation (A.D.), UCB-Celltech (C.D.S.), EPSRC (Z.G., Y.A.L.), and CRUK (Z.G.) for funding, and Profs V. Gouverneur and C. J. Schofield for helpful discussions. B.G.D. is a Royal Society Wolfson Merit Award recipient.

Abstract

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Building with PEGs: PEG–boronic acids, in the presence of simple Pd sources, are capable of acting as direct and effective Suzuki reagents in 70–98 % yield. When combined with non-natural amino acids, they allow efficient and direct, site-selective PEGylation of proteins at predetermined positions under biologically compatible conditions without the need for exogenous ligands.

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